Pharmaceutical formulation, its use, and method for its manufacture

Abstract

A pharmaceutical formulation of a calcium salt and a dry plant extract in the form of a coated tablet, in which the formulation has a core of at least one dry plant extract, enveloped by at least one coating of at least one calcium salt. The plant extracts for the core may be selected from: Vitex agnus castus (chaste tree); Belamcanda chinensis (leopard lily); Cimicifuga racemosa (black cohosh); Trifolium pratense L. (purple trefoil); Oenothera biennis hom. (primrose); Glycine soja (soy bean); Serenoa repens (saw-palmetto); Urtica dioica (stinging nettle), in particular its root; Cucurbita pepo (pumpkin), in particular its seed; Pygeum africanum; as well as suitable mixtures of these. Methods for the use of the formulation in treating osteoporosis and for manufacturing the formulation are provided.

Description

FIELD OF THE INVENTION[0001]The present invention relates to a pharmaceutical formulation of a calcium salt and a dry plant extract, its use in the treatment of osteoporosis, and a method for its manufacture.BACKGROUND TO THE INVENTION[0002]17β-estradiol, which is naturally formed in the ovaries [also referred to as E2], has a general proliferation-enhancing action in humans and animals. In addition to controlling the female cycle, it has, i. a., a homeostatic effect on the metabolism of the bone, while also preventing the formation of atherotic plaques on vessel endothelia.[0003]During menopause, estradiol levels decrease due to cessation of ovarial function. In the absence of sufficiently high estradiol levels in the blood, the activity of the osteoclasts, and thus breakdown of the bone mass—so-called “osteoporosis”—predominates in the bone tissue, which is accompanied by an increased risk of skeletal breakage.[0004]In recent times it was found that this syndrome of osteoporosis b...

AI Technical Summary

Problems solved by technology

In the absence of sufficiently high estradiol levels in the blood, the activity of the osteoclasts, and thus breakdown of the bone mass—so-called “osteoporosis”—predominates in the bone tissue, which is accompanied by an increased risk of skeletal breakage.

Administration of estrogens such as, e. g., 17β-estradiol or the chemical derivatives thereof is, however, accompanied by the known grave side effects of uterotrophic effect, increased risk of thrombo-embolism, weight gain, and the like.

Plant extracts have been frequently used that exhibit the desired action of osteoporosis prophylaxis, but not, however, the undesirable uterotrophic effects.

Simple admixture to a calcium effervescent tablet mass, however, is foiled by the high sensitivity of the dry extracts to acids in an aqueous medium on the one hand, and by the poor water solubility of many dry extracts in an acidic medium on the other hand.

Moreover the humidity-sensitive effervescent masses are imperiled by the highly hygroscopic dry extracts.

Moreover the stability of such gelatin capsules is not warranted, for it is reported in literature, e. g., that instances of crosslinking with the gelatin occur when plant extracts are encapsulated in gelatin, and significant changes of the ingredients result from water absorption by the dry extract.

As was mentioned above, significant calcium contents of 500 mg Ca2+ and more, together with the relatively large amounts of auxiliaries for dragée manufacture, would result in large dragée sizes and weights which would not be acceptable to patients.